thio-Miltefosine

thio-Miltefosine is a sulfur-containing derivative of miltefosine. Miltefosine is an inhibitor of phosphocholine cytidylyl transferase (CTP) and has antimetastatic properties. At concentrations of 3 and 25 µM, miltefosine inhibits proliferation of HaCaT cells (immortalized human keratinocyte cell line) by 50% and 94%, respectively. The mechanism of action of miltefosine is not well established, but the antiproliferative effect may be mediated by an increase in cellular ceramide which results in apoptosis. Treatment of cells with 25 µM miltefosine results in a 53% increase in ceramide concentration relative to control. Miltefosine is more than 90% effective in eradicating visceral infections of Leishmania species (kala azar), although the mechanism of this antiprotozoal activity is also poorly understood. The pharmacology of thio-miltefosine has not been published.